TMP269 NEW
Price | $66 | $97 | $164 |
Package | 2mg | 5mg | 10mg |
Min. Order: | |
Supply Ability: | 10g |
Update Time: | 2024-11-15 |
Product Details
Product Name: TMP269 | CAS No.: 1314890-29-3 |
Purity: 99.06% | Supply Ability: 10g |
Release date: 2024/11/15 |
Product Introduction
Bioactivity
名稱 | TMP269 |
描述 | TMP269 is an effective, specific class IIa HDAC inhibitor for HDAC4 (IC50: 157 nM), HDAC5 (IC50: 97 nM), HDAC7 (IC50: 43 nM), and HDAC9 (IC50: 23 nM), respectively. |
細(xì)胞實(shí)驗(yàn) | Human CD4+ T cells are isolated from whole blood via negative selection according to manufacturer's instructions (RosetteSep Human CD4+ T cell enrichment kit), re-suspended in T-cell culture medium (10% FBS, 2 mM L-glutamine, 1 mM pyruvate, 10 mM HEPES, 10 U/10 mg penicillin/streptomycin, 0.5% DMSO in RPMI) and plated at 50,000 cells/well with IL-2 (10 BRMP units/mL) and 100,000 human T-expander Dynabeads for 72 h. Determination of mitochondrial function or cell viability is done according to manufacturer's instructions (Cell Proliferation Assay Kit I (MTT)) and is represented as a percent of control (no inhibitor) wells.(Only for Reference) |
激酶實(shí)驗(yàn) | HDAC selectivity assays: Dose-response studies are done with ten concentrations in a threefold dilution series from a maximum final compound concentration of 100 μM in the reaction mixture and are conducted at Reaction Biology Corp. All assays are based on the same principle as the HDAC9 assay described above: the deacetylation of acetylated or trifluoroacetylated lysine residues on fluorogenic peptide substrates by HDAC. HDAC1, HDAC2, HDAC3, HDAC6, HDAC10 and HDAC11 used a substrate based on residues 379-382 of p53 (Arg-His-Lys-Lys(Ac)). For HDAC8, the diacetylated peptide substrate, based on residues 379–382 of p53 (Arg-His-Lys(Ac)-Lys(Ac)), is used. HDAC4, HDAC5, HDAC7 and HDAC9 assays used the class IIa HDAC–specific fluorogenic substrate (Boc-Lys(trifluoroacetyl)-AMC). All reactions are done with 50 μM HDAC substrate in assay buffer (50 mM Tris-HCl, pH 8.0, 137 mM NaCl, 2.7 mM KCl, 1 mM MgCl2, 1 mg/mL BSA) containing 1% DMSO final concentration; incubated for 2 h at 30 °C; and developed with trichostatin A and trypsin. |
體內(nèi)活性 | TMP269 (10 μM) does not affect mitochondrial activity and/or the activity of human CD4+ T cells and can be used to identify endogenous substrates of class IIa HDAC enzymes. In IEC-18 small intestinal epithelial cells, TMP269 inhibits cellular processes, DNA synthesis, and proliferation induced by the activation of G protein-coupled receptor/PKD1 signaling. |
存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | DMSO : 93 mg/mL (180.8 mM) Ethanol : 2 mg/mL (3.88 mM), Heating is recommended. H2O : < 1 mg/mL (insoluble or slightly soluble) |
關(guān)鍵字 | Inhibitor | TMP-269 | HDAC | TMP 269 | Histone deacetylases | TMP269 | inhibit |
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相關(guān)庫 | NF-κB 通路分子庫 | DNA 損傷和修復(fù)分子庫 | 抗胰腺癌化合物庫 | 經(jīng)典已知活性庫 | 表觀遺傳庫 | 抗乳腺癌化合物庫 | 抑制劑庫 | NO PAINS 化合物庫 | 抗衰老化合物庫 | 已知活性化合物庫 |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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